@article{oai:repo.qst.go.jp:00044311,
 author = {Haradahira, Terushi and Zhang, Ming-Rong and Maeda, Jun and Okauchi, Takashi and Kida, Takayo and Kawabe, Koichi and Sasaki, Shigeki and Suhara, Tetsuya and Suzuki, Kazutoshi and 原田平 輝志 and 張 明栄 and 前田 純 and 岡内 隆 and 佐々木 茂貴 and 須原 哲也 and 鈴木 和年},
 issue = {2},
 journal = {Chemical & Pharmaceutical Bulletin},
 month = {},
 note = {4-Acetoxy derivative(1) of L-703,717, a high-affinity (IC50=4.5nM) antagonist for the glycine site of NMDA receptors, was synthesized and its brain uptake was examined using a carbon-11 labeled analog ([11C]1).Initial radioactivity in the brain after intravenous injection of [11C]1 was a 2-fold that of [11C]L-703,717in mice.Rapid bioconversion of[11C]1 into [11C]L-703,717 was demonstrated by metabolite analyses of rat brain after [11C]1 injection. Ex vivo autoradiography of [11C]1 in rat brain showed the same cerebellar localization of radioactivity as [11C]L-703,717.These results indicate that 1 is a promising pharmacological tool as a prodrug of L-703,717 with improved BBB permeability.},
 pages = {147--150},
 title = {A Prodrug of NMDA/Glycine Site Antagonist, L-703,717, with Improved BBB Permeability: 4-Acetoxy Derivative and Its Positron-Emitter Labeled Analog},
 volume = {49},
 year = {2001}
}